Analysis of the effect of a 2-(trifluoromethyl)-1H-benzimidazole derivative on Trichinella spiralis muscle larvae

被引：13

作者：

Matadamas-Martinez, Felix ^{[1
,2
]}

Nogueda-Torres, Benjamin ^{[2
]}

Hernandez-Campos, Alicia ^{[3
]}

Hernandez-Luis, Francisco ^{[3
]}

Castillo, Rafael ^{[3
]}

Mendoza, Guillermo ^{[4
,5
]}

Ambrosio, Javier R.

Andres-Antonio, Gabriela ^{[1
]}

Yepez-Mulia, Lilian ^{[1
]}

机构：

[1] IMSS, Ctr Med Nacl Siglo 21, UIMEP Pediat, Mexico City 067206, DF, Mexico

[2] IPN, Escuela Nacl Ciencias Biol, Dept Parasitol, Mexico City 11340, DF, Mexico

[3] Univ Nacl Autonoma Mexico, Fac Quim, Dept Farm, Mexico City 04510, DF, Mexico

[4] Univ Nacl Autonoma Mexico, Fac Med, Dept Bioquim, Mexico City 04510, DF, Mexico

[5] Univ Nacl Autonoma Mexico, Fac Med, Dept Microbiol & Parasitol, Mexico City 04510, DF, Mexico

来源：

VETERINARY PARASITOLOGY | 2013年 / 194卷 / 2-4期

关键词：

Trichinella spiralis; Benzimidazole derivative; Anthelminthic activity; Proteomic analysis;

D O I：

10.1016/j.vetpar.2013.01.054

中图分类号：

R38 [医学寄生虫学]; Q [生物科学];

学科分类号：

07 ; 0710 ; 09 ; 100103 ;

摘要：

Albendazole and mebendazole are widely used in the treatment of trichinellosis; however, chemotherapy failure has been reported. In an effort to develop new anthelminthic compounds, we examined a previously synthesized 2-(trifluoromethyl)-1H-benzimidazole derivative (1) that showed good in vitro activity against Trichinella spiralis muscle larvae but low in vivo efficacy. In order to improve the solubility of compound 1, an inclusion complex with 2-hydroxypropyl-beta-cyclodextrin (1/HP-beta CD) was prepared. When 1/HP-beta CD was tested in vivo, it significantly reduced the ML burden (84%). In addition, a proteomic analysis of T. spiralis ML treated with 1 revealed significant changes in the expression levels of proteins involved in energy metabolism and the cytoskeleton of the parasite. Compound (1) also induced extensive ultrastructural changes in the cuticle, hypodermis and midgut of the parasite. (C) 2013 Elsevier B.V. All rights reserved.

引用

页码：193 / 197

页数：5

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